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In addition to the ESIs identified
2020-11-17

In addition to the ESIs identified that target both EPAC1 and EPAC2, ESI-05 and ESI-07 were identified as compounds that selectively antagonise EPAC2, displaying almost no inhibition of EPAC1 at concentrations up to 100μM [99]. Both compounds were effective inhibitors EPAC2 GEF activity towards Rap1
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br Structure and function of EPAC
2020-11-17

Structure and function of EPAC isoforms EPACs are guanine nucleotide exchange factors (GEFs) for the Ras-like GTPases Rap1 and Rap2 [9]. There are two mammalian EPAC isoforms, EPAC1 and EPAC2 1, 2 (Figure 1). Whereas EPAC1 displays a wide tissue distribution, the expression of EPAC2 is more restr
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br Acknowledgements The authors thank
2020-11-17

Acknowledgements The authors thank Drs. C. Klein, I. Canisso and A. Claes with assistance in obtaining tissues. Supported by the Albert G. Clay Endowment, University of Kentucky. Introduction Neoplastic cells often develop drug resistance during tumor progression or cancer treatment (Turner a
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Enhanced responses to varying concentrations of bronchoconst
2020-11-16

Enhanced responses to varying concentrations of bronchoconstrictors, such as MCh, and airway obstruction are characteristic of Colistin Methanesulfonate sodium salt and common to other clinical states, including chronic obstructive pulmonary disease, lung transplantation, and infection- or chemical
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br EBI structure and expression The gene encoding
2020-11-16

EBI2 structure and expression The gene encoding EBI2 was originally identified together with EBI1 (CCR7) as the most highly upregulated gene in Epstein–Barr virus-infected Burkitt's lymphoma cells [18]. EBI2 belongs to the rhodopsin-like subfamily of seven transmembrane GPCRs [19]. Although it is
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br EBI structure and expression The gene encoding
2020-11-16

EBI2 structure and expression The gene encoding EBI2 was originally identified together with EBI1 (CCR7) as the most highly upregulated gene in Epstein–Barr virus-infected Burkitt's lymphoma cells [18]. EBI2 belongs to the rhodopsin-like subfamily of seven transmembrane GPCRs [19]. Although it i
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MuRF interacts with four and a half LIM
2020-11-16

MuRF3 interacts with four-and-a-half LIM domain (FHL2) and γ-filamin leading to their degradation via UPS [64]. Conversely, abnormal aggregation of these proteins was observed in mice lacking MuRF3. Moreover, MuRF3-/- mice were found more prone to cardiac rupture after acute myocardial infarction (A
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AEB071 We recently reported that the information about the e
2020-11-16

We recently reported that the information about the electronic density obtained from a QTAIM analysis is useful to describe the molecular interactions that stabilize and destabilize the different complexes L-R [13], [14], [15]. Specifically in our previous work reported for DHFR inhibitors, the QTAI
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MTX and MTXPGs block the activity of the key enzyme
2020-11-16

MTX and MTXPGs block the activity of the key enzyme DHFR (Fig. 1), which converts folates to their active forms – dihydrofolate (DHF) and tetrahydrofolate (THF). MTXPGs also potently inhibit thymidylate synthase (TS). Furthermore, during dTMP synthesis, TS utilizes the cofactor 5,10-methylene THF, w
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ApicomplexansApicomplexans are unicellular and spore forming
2020-11-16

ApicomplexansApicomplexans are unicellular and spore-forming obligate intracellular parasites that occupy diverse host niches (Mogi and Kita 2010). They have remodeled mitochondrial carbon and energy metabolism through reductive evolution. The development of novel drugs is now a very serious challen
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ApicomplexansApicomplexans are unicellular and spore forming
2020-11-16

ApicomplexansApicomplexans are unicellular and spore-forming obligate intracellular parasites that occupy diverse host niches (Mogi and Kita 2010). They have remodeled mitochondrial carbon and energy metabolism through reductive evolution. The development of novel drugs is now a very serious challen
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Agglutinin like sequence ALS gene is well
2020-11-16

Agglutinin-like sequence (ALS) gene is well-characterized gene family in candidiasis due to its importance in pathogenicity of C albicans. Previously, C. albicans ALS1 gene product was reported as cell surface protein that mediates adherence to endothelial and epithelial Amyloid β-Peptide (1-42) in
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We thank Dr Hongqiang Qin at Dalian
2020-11-16

We thank Dr. Hongqiang Qin at Dalian Institute of Chemical Physics, Chinese Academy of Sciences for technical assistance in mass-spectrometric analysis. We thank Prof. Quentin Liu at Dalian Medical University and Prof. Qiang Shen at M.D. Anderson Cancer Center for helpful discussion and comments. Dr
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In a previous study we reported
2020-11-16

In a previous study we reported that the systemic administration of the α1-adrenergic receptor antagonist prazosin attenuates the deficit in SR 1555 hydrochloride synthesis reward function associated with precipitated nicotine withdrawal (Bruijnzeel et al., 2010). One of the aims of the present exp
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br Experimental section br Results br Discussion In our prev
2020-11-16

Experimental section Results Discussion In our previous work (Rashidi et al., 2018) we isolated a novel glucarpidase whose raised APY29 did not cross-react with the one in clinical use. In principle, therefore, it would be possible to delay the production of antibodies in a patient by alter
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